. Author manuscript; available in PMC: 2025 May 27.

Published in final edited form as: J Med Chem. 2024 Jul 19;67(15):12534–12552. doi: 10.1021/acs.jmedchem.4c00411

Table 4.

EC₅₀ values for prioritized compounds determined in a cellular NanoBRET target engagement assay. See Table S2 for the complete data set. n.d. = not determined.

	EC₅₀ [nM]
cpd ID	EPHA2	EPHA4	GAK	ABL1	FGFR1	FLT1
23	470 ± 31	450 ± 140	20 ± 5.7	27000 ± 210	3100 ± 870	13000 ± 5400
54	370 ± 68	84 ± 32	160 ± 29	2700^*	1200 ± 230	13000 ± 130
55	260 ± 73	57 ± 23	27 ± 5.6	>50000	18000 ± 1900	33000 ± 3600
56	440 ± 0.99	250 ± 57	40^*	30000 ± 2300	2000^*	7500^*
58	250^*	190 ± 45	n.d.	6400^*	470^*	1100^*
61	340 ± 81	37 ± 12	33 ± 4.9	8400^*	7600 ± 1100	17000 ± 2300
75	1600 ± 380	37 ± 12	24 ± 3.4	>50000	34000 ± 11000	42000 ± 5700
78	470^*	n.d.	30^*	17000^*	n.d.	n.d.
79	1400 ± 290	60 ± 13	31 ± 2.9	32000^*	9800 ± 1900	23000 ± 2600
LDN-211904	270^*	48 ± 6.3	−0.4% binding @ 1 μM	49000^*	>50000^*	>50000^*

Mean of one experiment performed in technical duplicates